Bulletin of the Korean Chemical Society

Korean Chemical Society (대한화학회)
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A Blood-brain Barrier Permeable Derivative of 5-Fluorouracil: Preparation, Intracellular Localization, and Mouse Tissue Distribution

  • Im, Jung-Kyun (Department of Chemistry, Pohang University of Science and Technology) ;
  • Biswas, Goutam (Department of Chemistry, Pohang University of Science and Technology) ;
  • Kim, Wan-Il (Department of Life Science, Pohang University of Science and Technology) ;
  • Kim, Kyong-Tai (Department of Life Science, Pohang University of Science and Technology) ;
  • Chung, Sung-Kee (Department of Chemistry, Pohang University of Science and Technology)
  • Received : 2010.12.07
  • Accepted : 2011.01.05
  • Published : 2011.03.20
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Abstract

5-Fluorouracil (5-FU), an anticancer agent was covalently attached to the recently developed sorbitol-based G8 transporter, and the conjugate (7) with FITC was found to have an affinity toward mitochondria and to readily cross BBB to gain an entry into mouse brain. Measured by $IC_{50}$, the conjugate (9) without the fluorophore showed enhanced cytotoxic activity toward two types of multidrug-resistant cell lines. These results strongly suggest that the sorbitol-based G8 transporter can be utilized as a good CNS delivery vector.

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References

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